Abstract:
Sublingual tablets are gaining popularity over conventional tablets due to their convenience in
administration and suitability for elderly and children who have swallowing difficulties. The aim of this study was to
formulate Chlorpheniramine Maleate (CPM) sublingual tablets to achieve rapid onset of action. CPM is a first
generation antihistamines, undergoes first pass metabolism in liver. Sublingual dosage forms bypass the metabolism
of CPM in liver and so improve the drug bioavailability. The novel ternary phase developed by co-processed
superdisintegrants via solvent evaporation method using crospovidone, croscarmellose and sodium starch glycolate
in different ratios (1:1:1, 3:1:1, 1:3:1and 1:1:3) were prepared. The pre-compression parameters (angle of repose,
Hausner ratio and Carr’s index) of the prepared co-processed superdisintegrants were evaluated in comparison to
physical mixture of superdisintegrants. The developed co-processed formulae were compared with those the
corresponding physical mixtures and individual superdisintegrant sublingual tablets. The tablets were evaluated for
its disintegration time, wetting time, in-vitro dispersion time as well as hardness, weight variation, friability, drug
content and in-vitro dissolution study. Among all the designed formulations, the formulations CP1 and PM1
containing 4% w/w co-processed and physical mixture of superdisintegrant respectively (1:1:1 mixture of
crospovidone, croscarmellose and sodium starch glycolate) were considered to be best formulations, which showed
the shortest disintegration time (6.29 and 6.31 sec), in-vitro dispersion time (18.67 and 18.83 sec) and wetting time
(12.47 and 12.58 sec) respectively. As well as these promising formulae showed highest drug release (100 and 97.52
%) within two min. Finally, the promising formulae were compared with CPM sublingual tablet prepared using
commercially available co-processed mixture of excipients containing superdisintegrant (PharmaburstTM500). There
were significance differences in disintegration time, in-vitro dispersion time, wetting time and in vitro drug release
(p<0.001) using ANOVA-one way test.
